Transpl Infect Dis
Laboratory of Viral Diseases, Wadsworth Center, New York State Department of Health, Albany, NY, USA.
Published: June 2021
Few treatment options are available for oseltamivir-resistant influenza. It has been proposed that baloxavir can be effective in this setting due to its distinct mechanism of action but clinical experience is lacking for immunocompromised patients. We report two such cases treated with baloxavir after failure of oseltamivir and detection of oseltamivir resistance mutations. Baloxavir/zanamivir combination therapy was effective in one patient, but persistent viral shedding was noted with baloxavir monotherapy in the other patient.
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http://dx.doi.org/10.1111/tid.13542 | DOI Listing |
J Med Chem
December 2024
Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, Jinan, Shandong 250012, P. R. China.
Inspired by our previous finding that targeting the 150-cavity with a multisite-binding strategy emerged as an effective approach to obtain more potent and selective neuraminidase (NA) inhibitors against influenza virus, we present here the design, synthesis, and optimization of novel boron-containing N-substituted oseltamivir (OSC) derivatives. Exploratory structure-activity relationship (SAR) studies led to the identification of compounds and as the most potent NA inhibitors, surpassing OSC in potency against both wild-type group-1 NAs and oseltamivir-resistant NAs. These compounds demonstrated significant antiviral activity against several wild-type strains and H1N1pdm09 strains (EC = 0.
View Article and Find Full Text PDFChem Biodivers
November 2024
Key Laboratory of Tropical Biological Resources of Ministry of Education, School of Pharmaceutical Sciences, Hainan University, Haikou, Hainan, China.
ACS Cent Sci
August 2024
Department of Chemistry, College of Natural Sciences, Seoul National University, Seoul 08826, Republic of Korea.
We present orally administrable prodrugs (s) of guanidino oseltamivir carboxylate () based on guanidine cyclic diimide (GCDI) to treat influenza viruses. By concealing the guanidine group, which significantly limits the intestinal absorption, its prodrugs s demonstrate dramatic improvement of oral bioavailability. The most promising antiviral substance readily forms covalent adducts with serum proteins via a degradable linker after the intestinal absorption.
View Article and Find Full Text PDFViruses
August 2024
Infectious Diseases Research Center of Niigata University in Myanmar (IDRC), Graduate School of Medical and Dental Sciences, Niigata University, Niigata 951-8510, Japan.
J Ethnopharmacol
January 2025
NMPA Key Laboratory for Research and Evaluation of Drug Metabolism & Guangdong Provincial Key Laboratory of New Drug Screening & Guangdong-Hongkong-Macao Joint Laboratory for New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, PR China. Electronic address:
Ethnopharmacological Relevance: Jinye Baidu granules (JYBD) have been used to treat acute respiratory tract infections and demonstrated clinical efficacy for the treatment of emerging or epidemic respiratory viruses such as SARS-CoV-2 and influenza virus.
Aim Of The Study: This study is to investigate the antiviral effect of JYBD against influenza A viruses (IAV) in vitro and in vivo and elucidate its underlying mechanism.
Materials And Methods: Ultra-high-performance liquid chromatography connected with Orbitrap mass spectrometer (UHPLC-Orbitrap MS) was employed to describe the chemical profile of JYBD.
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